2025 Medicinal Chemistry Reviews
Editor(s):
Volume 60
Publication Date (Web):November 21, 2025
1 Genentech, South San Francisco, California, U.S.A.
2 Gilead Sciences, Foster City, California, U.S.A.
ISBN13: 9798993118116
eISBN: 9798993118109
DOI: 10.1021/mc-2025-vol60
Joachim Rudolph and Will Watkins, Editors-In-Chief, the ACS Division of Medicinal Chemistry, and the American Chemical Society are pleased to announce the publication of 2025 Medicinal Chemistry Reviews, Volume 60 in the series. Become a member of the ACS Division of Medicinal Chemistry now to access the electronic version of Medicinal Chemistry Reviews at no cost in the Resources section. As of 2022, ACS eBooks collections now include Medicinal Chemistry Reviews, an outstanding annual volume produced by the ACS Division of Medicinal Chemistry, providing timely and critical reviews of important topics in medicinal chemistry. Prior year volumes can be obtained from the ACS Division of Medicinal Chemistry.
Table of Contents, Contributor List, Preface
Chapter
frnt, i-xxiiiDOI: 10.1021/mc-2025-vol60.frnt
MOLECULES, MENTORS, AND MOMENTS THAT MATTERED
Wendy Young
Chapter
1, 1-41DOI: 10.1021/mc-2025-vol60.ch01
THE PRIVILEGE OF MAKING A DIFFERENCE IN DEVELOPING AND DELIVERING MEDICINES
Taiyin Yang
Chapter
2, 43-55DOI: 10.1021/mc-2025-vol60.ch02
EXPLORING THE THERAPEUTIC LANDSCAPE OF MONOACYLGLYCEROL LIPASE (MAGL) INHIBITORS: ADVANCES IN SMALL-MOLECULE DISCOVERY
Fionn O’Hara - ,
Bernd Kuhn - , and
Uwe Grether
Chapter
3, 59-81DOI: 10.1021/mc-2025-vol60.ch03
SMALL-MOLECULE M1 AND M4 ACTIVATORS FOR THE TREATMENT OF COGNITIVE IMPAIRMENT AND PSYCHOSIS
Brian Laforteza - ,
Michael Rombola - , and
Usha Viswanathan
Chapter
4, 83-107DOI: 10.1021/mc-2025-vol60.ch04
RECENT ADVANCES IN SMALL-MOLECULE THERAPEUTICS TARGETING NEUROINFLAMMATION
René Johannes Rahimoff - and
Marko Nesic
Chapter
5, 109-137DOI: 10.1021/mc-2025-vol60.ch05
SMALL-MOLECULE AGONISTS OF THYROID HORMONE RECEPTOR BETA (THR-β)
David C. McGowan - and
Xuan G. Luong
Chapter
6, 141-163DOI: 10.1021/mc-2025-vol60.ch06
LYSOPHOSPHATIDIC ACID RECEPTOR 1 (LPA1) ANTAGONISTS
Peter T. W. Cheng - and
James R. Corte
Chapter
7, 167-193DOI: 10.1021/mc-2025-vol60.ch07
SMALL-MOLECULE MODULATORS OF CYTOKINE-RECEPTOR INTERACTIONS
Wenying Angela Liu - and
Ge Zou
Chapter
8, 195-215DOI: 10.1021/mc-2025-vol60.ch08
RECENT DISCOVERY EFFORTS TARGETING INHIBITION OF HEMATOPOIETIC PROTEIN KINASE 1 (HPK1) AS A NOVEL CANCER IMMUNOTHERAPY
Rebecca A. Gallego - ,
Neelu Kaila - , and
David Ciccone
Chapter
9, 219-241DOI: 10.1021/mc-2025-vol60.ch09
RECENT ADVANCES IN WERNER HELICASE (WRN) INHIBITION FOR MICROSATELLITE INSTABILITY-HIGH CANCERS
Lindsey G. DeRatt - ,
Francis W. Hunter - , and
Scott D. Kuduk
Chapter
10, 243-271DOI: 10.1021/mc-2025-vol60.ch10
ANTIBODY-DRUG CONJUGATES IN ONCOLOGY: RECENT ACHIEVEMENTS AND CURRENT CHALLENGES
Timothy B. Lowinger - and
Dorin Toader
Chapter
11, 273-296DOI: 10.1021/mc-2025-vol60.ch11
ADVANCES IN SMALL-MOLECULE–BASED THERAPIES AGAINST HUMAN PATHOGENIC FREE-LIVING AMOEBAE
Julia M. Pomeroy - ,
Seoyoung Kim - , and
Jennifer E. Golden
Chapter
12, 301-325DOI: 10.1021/mc-2025-vol60.ch12
NEW KIDS ON THE BLOCK: PROXIMITY-BASED MODALITIES AS ANTIVIRAL THERAPIES
Isaac D. Falk - and
Rhiannon Thomas-Tran
Chapter
13, 327-345DOI: 10.1021/mc-2025-vol60.ch13
EMERGING MEDICINAL CHEMISTRY APPROACHES TO MODULATE TRANSCRIPTIONAL ACTIVITY BY ACETYLATION
Victoria D. Kutilek - ,
Tamara D. Hopkins - , and
Margaret Biddle
Chapter
14, 349-367DOI: 10.1021/mc-2025-vol60.ch14
RECENT ADVANCES, NEW DEVELOPMENTS, AND EMERGING OPPORTUNITIES IN DNA-ENCODED LIBRARY TECHNOLOGY
Christian Nilewski - ,
Moreno Wichert - , and
James Hunter
Chapter
15, 369-397DOI: 10.1021/mc-2025-vol60.ch15
A DRUG HUNTER’S APPROACH TO MOLECULAR GLUES
Daniel S. La - ,
Christopher G. Nasveschuk - , and
Adam M. Gilbert
Chapter
16, 399-427DOI: 10.1021/mc-2025-vol60.ch16
LEVERAGING PROTEIN TURNOVER IN DRUG DISCOVERY: A PRACTICAL GUIDE
Jitao David Zhang - ,
Neil John Parrott - ,
Martin Ebeling - ,
Miro Eigenmann - ,
Kenichi Umehara - , and
Holger Fischer
Chapter
17, 429-467DOI: 10.1021/mc-2025-vol60.ch17
NAVIGATING CHALLENGES IN ORAL HETEROBIFUNCTIONAL DEGRADERS: INSIGHTS AND STRATEGIES FOR EARLY-STAGE PROJECTS
Tezcan Guney - ,
Anh T. Tran - , and
Katie Stamp
Chapter
18, 471-499DOI: 10.1021/mc-2025-vol60.ch18
DEVELOPMENT OF E3 LIGANDS TO ENABLE NEXT-GENERATION DEGRADERS
Karli Holman - and
Westley Tear
Chapter
19, 501-535DOI: 10.1021/mc-2025-vol60.ch19
CASE HISTORY: TRUQAP® (CAPIVASERTIB) WITH FULVESTRANT FOR THE TREATMENT OF HR-POSITIVE, HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER WITH PIK3CA/AKT1/PTEN-ALTERATIONS
Jason G. Kettle - ,
Elza C. de Bruin - ,
Andrew Foxley - ,
Gaia Schiavon - , and
Simon T. Barry
Chapter
20, 539-567DOI: 10.1021/mc-2025-vol60.ch20
CASE HISTORY: DISCOVERY AND DEVELOPMENT OF THE PI3Kδ-SELECTIVE INHIBITOR JOENJA® (LENIOLISIB, CDZ173) AS A TARGETED THERAPY FOR PATIENTS WITH ACTIVATED PI3Kδ SYNDROME (APDS)
Klemens Hoegenauer - ,
Nicolas Soldermann - ,
Christoph Burkhart - , and
Christoph Kalis
Chapter
21, 569-585DOI: 10.1021/mc-2025-vol60.ch21
NEW CHEMICAL ENTITIES ENTERING PHASE III TRIALS IN 2024
David W. Lin - ,
Megan Armstrong - ,
Jennifer Jiang - ,
Renyu Guo - ,
Christiana N. Teijaro - , and
Tobias Sandmeier
Chapter
22, 587-605DOI: 10.1021/mc-2025-vol60.ch22
TO MARKET, TO MARKET—2024: SMALL MOLECULES
Sarah Anthony - ,
Erika Araujo - ,
Björn Bartels - ,
Marco Brandstaetter - ,
Christopher Bungard - ,
Georgette Castanedo - ,
T. G. Murali Dhar - ,
Natalie Holmberg-Douglas - ,
Renyu Guo - ,
Jeremy Richter - ,
Scott H. Watterson - ,
Dennis C. Koester - ,
Brian León - ,
James R. Manning - ,
J. Robert Merritt - ,
Kevin M. Peese - ,
Samantha Shockley - ,
Meng Yao Zhang - ,
Anh T. Tran - ,
Wei Zhao - , and
Joanne J. Bronson
Chapter
23, 607-807DOI: 10.1021/mc-2025-vol60.ch23
TO MARKET, TO MARKET—2024: MACROMOLECULAR THERAPEUTICS
Shion A. Lim - ,
Nicholas J. Agard - ,
James R. Byrnes - ,
Ryan L. Kelly - ,
Santhosh K. Thatikonda - ,
Benjamin N. Bell - ,
Diana J. Wang - ,
Si-Jie Chen - ,
Ivelisse Cruz-Torres - ,
Anna M. Gram - ,
Katarina Pance - , and
Brett R. Robison
Chapter
24, 809-909DOI: 10.1021/mc-2025-vol60.ch24